Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Ajit Jadhav"'
Autor:
Hongchao Zheng, Andrew L. McIver, Surendra Karavadhi, Adam Yasgar, William J. Moore, Li Liu, Zhuyin Li, Carleen Klumpp-Thomas, Ajit Jadhav, Natalia J. Martinez, Kyle R. Brimacombe, Mindy I. Davis, Wei Zhao, Daniel J. Urban, Stephen V. Frye, Anton Simeonov, Xiaodong Wang, Samarjit Patnaik, Rajan Pragani, Mark J. Henderson, Weihe Zhang, Melinda G. Hollingshead, Min Shen, Qingyang Liu, Gordon M. Stott, Tobie D. Lee, Sam Michael, Matthew B. Boxer, Jason M. Rohde, Matthew D. Hall, Yuhong Fang, Joseph M. Covey, Dorian M. Cheff
Publikováno v:
J Med Chem
Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are oncogenic for a number of malignancies, primarily low-grade gliomas and acute myeloid leukemia (AML). We report a medicinal chemistry campaign around a 7,7-dimethyl-7,8-dihydro-2H-1λ(2)-q
Autor:
Matthew D. Hall, Xin Xu, Pranav Shah, Olivia W. Lee, Min Shen, Hu Zhu, Samarjit Patnaik, Ajit Jadhav
Publikováno v:
SLAS Discov
Fumarate hydratase (FH) is a metabolic enzyme that is part of the Krebs-cycle, and reversibly catalyzes the hydration of fumarate to malate. Mutations of the FH gene have been associated with fumarate hydratase deficiency (FHD), hereditary leiomyomat
Autor:
Matthew D. Hall, David J. Maloney, Amy Wang, Jeffrey W. Strovel, Makoto Yoshioka, Daniel J. Urban, Xin Xu, Shyh-Ming Yang, Pranav Shah, Ajit Jadhav, Steven Fletcher, Xin Hu
Publikováno v:
Bioorg Med Chem Lett
A new series of quinazoline-based analogs as potent bromodomain-containing protein 4 (BRD4) inhibitors is described. The structure-activity relationships on 2- and 4-position of quinazoline ring, and the substitution at 6-position that mimic the acet
Autor:
Paul M Will, Wenwei Huang, Stephan Meister, Dorjbal Dorjsuren, Anton Simeonov, Bryan T. Mott, Andrew T Girvin, Pranav Shah, David A. Fidock, Daniel C. Talley, Benjamin A Sigmon, Richard T. Eastman, Xin Xu, Sachel Mok, Leila S. Ross, Tomas Yeo, Daniel J. Jansen, Robert F. Campbell, Alexey V. Zakharov, Richard J. Sciotti, Carleen Klumpp-Thomas, Yevgeniya Antonova-Koch, Norman C. Waters, Juan J. Marugan, Norma Roncal, Elizabeth A. Winzeler, David J. Maloney, Kathryn J. Wicht, Ajit Jadhav, Hongmao Sun
Publikováno v:
Scientific Reports
Scientific Reports, Vol 11, Iss 1, Pp 1-16 (2021)
Scientific Reports, Vol 11, Iss 1, Pp 1-16 (2021)
The spread of Plasmodium falciparum parasites resistant to most first-line antimalarials creates an imperative to enrich the drug discovery pipeline, preferably with curative compounds that can also act prophylactically. We report a phenotypic quanti
Autor:
Douglas R. Davies, Gloria A. Benavides, Xin Hu, Jeffrey P. Norenberg, Somnath Jana, Ganesha Rai, Pavan Muttil, Larry A. Sklar, Katherine Pohida, Daniel J. Urban, Kabir, David M. Dranow, Andrew J. Flint, Leonard M. Neckers, Giuseppe L. Squadrito, David J. Maloney, William J. Moore, Victor M. Darley-Usmar, Elias C. Padilha, Ajit Jadhav, Matthew D. Hall, Kyle R. Brimacombe, Dorian M. Cheff, Anton Simeonov, Nitesh K. Kunda, Plamen P. Christov, Pranav Shah, Tamara Anderson, Dingyin Tao, Hu Zhu, Murali Cherukuri, Yuhong Fang, Shyh-Ming Yang, Gary A. Sulikowski, Gordon M. Stott, Donna F. Kusewitt, Tobie D. Lee, Chi V. Dang, Alex G. Waterson, Mark J. Henderson, Bryan T. Mott, Kwangho Kim, Michelle S. Johnson, Helen J. Hathaway, Nobu Oshima
Publikováno v:
J Med Chem
Lactate dehydrogenase (LDH) catalyzes the conversion of pyruvate to lactate, with concomitant oxidation of reduced nicotinamide adenine dinucleotide as the final step in the glycolytic pathway. Glycolysis plays an important role in the metabolic plas
Autor:
Matthew P. Jacobson, Nathan C. Gilbert, Wan-Chen Tsai, Adam Yasgar, Chakrapani Kalyanaraman, Michelle Armstrong, Melissa Standley, Anthony T. Iavarone, Amanda Ohler, David B. Neau, Ganesha Rai, Adam R. Offenbacher, Marcia E. Newcomer, Phillip Crews, Steve Perry, Anton Simeonov, Hsiau-Wei Lee, Ajit Jadhav, Theodore R. Holman
Publikováno v:
Bioorg Med Chem
Human epithelial 15-lipoxygenase-2 (h15-LOX-2, ALOX15B) is expressed in many tissues and has been implicated in atherosclerosis, cystic fibrosis and ferroptosis. However, there are few reported potent/selective inhibitors that are active ex vivo. In
Autor:
Eric J. Kuenstner, David M. Dranow, Victor M. Darley-Usmar, Gary A. Sulikowski, Douglas R. Davies, Hu Zhu, Ganesha Rai, William J. Moore, David J. Maloney, Anton Simeonov, Dorian M. Cheff, Ajit Jadhav, Chi V. Dang, Kyle R. Brimacombe, Shyh-Ming Yang, Andrew J. Flint, Leonard M. Neckers, Gordon M. Stott, Tobie D. Lee, Xin Hu, Katie Pohida, Christine Lukacs, Alex G. Waterson, Daniel J. Urban, Diane K. Luci, Bryan T. Mott, Gloria A. Benavides, Matthew D. Hall, Jennifer Kouznetsova
Publikováno v:
Journal of Medicinal Chemistry. 60:9184-9204
We report the discovery and medicinal chemistry optimization of a novel series of pyrazole-based inhibitors of human lactate dehydrogenase (LDH). Utilization of a quantitative high-throughput screening paradigm facilitated hit identification, while s
Autor:
Adam Yasgar, David J. Maloney, Leggy A. Arnold, Ganesha Rai, Anton Simeonov, Preetpal S. Sidhu, Ajit Jadhav, Kelly A. Teske, Premchendar Nandhikonda, Belaynesh Feleke
Publikováno v:
ACS Combinatorial Science. 19:646-656
We describe the parallel synthesis of novel analogs of GW0742, a peroxisome proliferator-activated receptor δ (PPARδ) agonist. For that purpose, modified reaction conditions were applied, such as a solid-phase palladium-catalyzed Suzuki coupling. I
Autor:
Shyh Ming Yang, David J. Maloney, Lita A. Freeman, Alisa Glukhova, Kelly A. Manthei, Louise Chang, Wenmin Yuan, Anna Schwendeman, Ajit Jadhav, Alan T. Remaley, John J.G. Tesmer, Bolormaa Baljinnyam
Publikováno v:
eLife
eLife, Vol 7 (2018)
eLife, Vol 7 (2018)
Lecithin:cholesterol acyltransferase (LCAT) and LCAT-activating compounds are being investigated as treatments for coronary heart disease (CHD) and familial LCAT deficiency (FLD). Herein we report the crystal structure of human LCAT in complex with a
Autor:
David J. Maloney, Daniel J. Urban, Shyh-Ming Yang, Makoto Yoshioka, Xin Hu, Jeffrey Strovel, Ajit Jadhav, Matthew D. Hall
Publikováno v:
Bioorg Med Chem Lett
Extensive optimization of quinazoline-based lead 8 is described. The structure-activity relationship studies indicate the S-configuration is preferred for the phenylmorpholine substitution. Together with incorporation of a (2-hydroxyl-2-methylpropyl)